The objective of this work is to demonstrate changes in properties and increase of biological activity of nicotinamide (NAM) substance for skin protectants activated by mechanical activation (MA). To assess the physical, chemical and biological properties of NAM were used biotesting by the Spirotox-method, direct and indirect optical methods (microscopy, laser diffraction), infrared spectroscopy, pH-metry. The results of the study showed an increase in biological activity, expressed in changes in the energy of activation of cell transition to the "dead cell" state on the example of biosensor Spirostomum ambiguum. Also we indicated an increase in the rate of the chemical process of dissolution of mechanoactivated molecular crystals of nicotinamide (NAM) expressed in the values of the first order rate constant. Mechanical activation at a high rate of NAM substance powder deformation has led to changes in physical, chemical and biological properties of the drug, which can be used in medicine to increase efficiency and reduce doses of pharmacotherapy. Keywords: nicotinamide (NAM), basal cell carcinoma (BCC), mechanical activation (MA), microscopy, laser diffraction, Spirotox method.